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Preparation of hydroxypropylmethyl cellulose-based porous matrix for gastroretentive delivery of gabapentin using the freeze-drying method
Authors:Ju-Young Kim  Sang-hyub Kim  Yun-Seok Rhee  Chun-Woong Park  Eun-Seok Park
Institution:1. School of Pharmacy, Sungkyunkwan University, Jangan-gu, Suwon, Gyeonggi-do, 440-746, Republic of Korea
2. College of Pharmacy and Research Institute of Pharmaceutical Sciences, Gyeongsang National University, Jinju, 660-751, Republic of Korea
3. College of Pharmacy, Chungbuk National University, Cheongju, 361-763, Republic of Korea
Abstract:The aims of the present study were to prepare hydroxypropylmethyl cellulose (HPMC)-based porous matrix tablets for gastroretentive drug delivery and to characterize their physicochemical properties. Gabapentin (GBP) was used as a model drug. Paste containing GBP, HPMC and water was molded and freeze-dried to prepare freeze-dried gastroretentive matrix tablet (FD-GRT). In vitro drug release and erosion studies were also performed. Although FD-GRT exhibited porous structure, they had good tablet strength and friability. Density of FD-GRT ranged from 0.402 to 0.509 g/cm3 and thus they could float on the medium surface without any lag time. FD-GRT was remained floated until the entire matrix erosion or end of drug release during in vitro release test. Release behavior of GBP could be modulated by the amount and the viscosity grade of HPMC. However, large amount and high viscosity of HPMC caused trouble in molding prior to freeze-drying. Addition of ethylcellulose could retard the release rate of GBP, with relatively low increase in viscosity of paste. Since pores generated by freeze drying imparted buoyancy for gastric retention to FD-GRT, additional materials for buoyancy was not necessary and FD-GRT had no lag time for buoyancy due to low density. Therefore it could be a promising tool for gastroretentive drug delivery.
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